IPI-145 (INK1197)PI3K-δ/PI3K-γ inhibitor CAS# 1201438-56-3 |
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1201438-56-3 | SDF | Download SDF |
| PubChem ID | 50905713 | Appearance | Powder |
| Formula | C22H17ClN6O | M.Wt | 416.86 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | IPI-145; INK1197 | ||
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one | ||
| SMILES | CC(C1=CC2=C(C(=CC=C2)Cl)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 | ||
| Standard InChIKey | SJVQHLPISAIATJ-ZDUSSCGKSA-N | ||
| Standard InChI | InChI=1S/C22H17ClN6O/c1-13(28-21-19-20(25-11-24-19)26-12-27-21)17-10-14-6-5-9-16(23)18(14)22(30)29(17)15-7-3-2-4-8-15/h2-13H,1H3,(H2,24,25,26,27,28)/t13-/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | IPI-145 is an orally bioavailable and highly selective inhibitor of PI3K-δ and PI3K-γ with IC50 values of 0.36 nM and 19.6 nM, respectively. | |||||
| Targets | PI3K-δ | PI3K-γ | ||||
| IC50 | 0.36 nM | 19.6 nM | ||||
IPI-145 (INK1197) Dilution Calculator
IPI-145 (INK1197) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3989 mL | 11.9944 mL | 23.9889 mL | 47.9777 mL | 59.9722 mL |
| 5 mM | 0.4798 mL | 2.3989 mL | 4.7978 mL | 9.5955 mL | 11.9944 mL |
| 10 mM | 0.2399 mL | 1.1994 mL | 2.3989 mL | 4.7978 mL | 5.9972 mL |
| 50 mM | 0.048 mL | 0.2399 mL | 0.4798 mL | 0.9596 mL | 1.1994 mL |
| 100 mM | 0.024 mL | 0.1199 mL | 0.2399 mL | 0.4798 mL | 0.5997 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IPI-145 (also known as INK1197), an isoquinolinone derivative, is a small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. Despite of preference for PI3K-δ and PI3K-γ, IPI-145 also inhibits other PI3K isoforms, PI3K-α and PI3K-β, to a lesser extent with IC50 of 1602 nM and 85 nM respectively.
Due to the essential role of PI3K-δ in the proliferation of B cell and T cell, IPI-145 exhibits potent anti-proliferative activity against both cells with IC50 of 0.5 nM and 9.5 nM respectively leading to inhibition of neutrophil migration and basophil activation.
Inhibition of immune function through IPI-145-induced PI3K-δ and PI3K-γ blockade potentiates its application in the treatment of multiple inflammatory, autoimmune and hematologic diseases.
References:
[1] Winkler DG1, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. doi: 10.1016/j.chembiol.2013.09.017. Epub 2013 Nov 7.
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